TRELSTAR- triptorelin pamoate injection, powder, lyophilized, for suspension
TRELSTAR- triptorelin pamoate
Actavis Pharma, Inc.
1 INDICATIONS AND USAGE
TRELSTAR is indicated for the palliative treatment of advanced prostate cancer [see Clinical Studies (14)].
2 DOSAGE AND ADMINISTRATION
2.1 Dosing Information
TRELSTAR must be administered under the supervision of a physician.
TRELSTAR is administered by a single intramuscular injection in either buttock. Dosing schedule depends on the product strength selected (Table 1). The lyophilized microgranules are to be reconstituted in sterile water . No other diluent should be used.
Table 1. TRELSTAR Recommended Dosing
Dosage 3.75 mg 11.25 mg 22.5 mg
Recommended dose 1 injection every 4 weeks 1 injection every 12 weeks 1 injection every 24 weeks
Due to different release characteristics, the dosage strengths are not additive and must be selected based upon the desired dosing schedule.
The suspension should be administered immediately after reconstitution.
As with other drugs administered by intramuscular injection, the injection site should be alternated periodically.
Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
2.2 Reconstitution Instructions for TRELSTAR
Please read the instructions completely before you begin.
Wash your hands with soap and hot water and put on gloves immediately prior to preparing the injection.
Place the vial in a standing upright position on a clean, flat surface that is covered with a sterile pad or cloth.
Remove the Flip-Off� button from the top of the vial, revealing the rubber stopper.
Disinfect the rubber stopper with an alcohol wipe. Discard the alcohol wipe and allow the stopper to dry.
Using a syringe fitted with a sterile 21-gauge needle, withdraw 2 mL sterile water for injection, and inject into the vial.
Shake well to thoroughly disperse particles to obtain a uniform suspension. The suspension will appear milky.
Slowly withdraw the entire contents of the reconstituted suspension into the syringe.
The suspension should be administered immediately after reconstitution.
Inject the patient in either buttock with the contents of the syringe
3 DOSAGE FORMS AND STRENGTHS
Injectable suspension: 3.75 mg, 11.25 mg, 22.5 mg.
4 CONTRAINDICATIONS
4.1 Hypersensitivity
TRELSTAR is contraindicated in individuals with a known hypersensitivity to triptorelin or any other component of the product, or other GnRH agonists or GnRH [see Warnings and Precautions (5.1 )].
4.2 Pregnancy
TRELSTAR may cause fetal harm when administered to a pregnant woman. Expected hormonal changes that occur with TRELSTAR treatment increase the risk for pregnancy loss and fetal harm when administered to a pregnant woman [see Use in Specific Populations ( 8.1) ]. TRELSTAR is contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus.
DESCRIPTION
TRELSTAR is a white to slightly yellow lyophilized cake. When reconstituted, TRELSTAR has a milky appearance. It contains a pamoate salt of triptorelin, a synthetic decapeptide agonist analog of gonadotropin releasing hormone (GnRH). The chemical name of triptorelin pamoate is 5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-tryptophyl-L-leucyl-L-arginyl-L-prolylglycine amide (pamoate salt). The empirical formula is C64 H82 N18 O13 � C23 H16 O6 and the molecular weight is 1699.9
The TRELSTAR products are sterile, lyophilized biodegradable microgranule formulations supplied as single dose vials. Refer to Table 5 for the composition of each TRELSTAR product.
12 CLINICAL PHARMACOLOGY
12.1 Mechanism of Action
Triptorelin is a synthetic decapeptide agonist analog of gonadotropin releasing hormone (GnRH). Comparative in vitro studies showed that triptorelin was 100-fold more active than native GnRH in stimulating luteinizing hormone release from monolayers of dispersed rat pituitary cells in culture and 20-fold more active than native GnRH in displacing 125 I-GnRH from pituitary receptor sites. In animal studies, triptorelin pamoate was found to have 13?fold higher luteinizing hormone-releasing activity and 21-fold higher follicle-stimulating hormone-releasing activity compared to the native GnRH
PATIENT COUNSELING INFORMATION
Instruct patients that they will likely experience an increase in serum testosterone levels following their initial injection. This may cause a worsening of their symptoms of prostate cancer during the first weeks of treatment. These symptoms may include bone pain, spinal cord injury, hematuria, and urethral or bladder outlet obstruction. This increase in serum testosterone levels and associated symptoms should decline 3 to 4 weeks following their injection. Use of drugs appropriate for alleviating the risk associated with the increase should be discussed with patients prior to administration of the products. Patients should also be informed about the increased risk of developing diabetes, myocardial infarction, sudden cardiac death and stroke in men in association with use of GnRH agonists.
Advise patients that allergic reactions, including serious allergic reactions, could occur and that serious reactions require immediate treatment. Patients should report any previous hypersensitivity reactions to triptorelin, or other GnRH agonists, or GnRH.
For all medical inquiries contact:
ACTAVIS
Medical Communications
Parsippany, NJ 07054 USA
1-800-272-5525
